Disease chemopreventive effects and molecular mechanisms of hydroxylated polymethoxyflavones

Recent increasing attention in research of polymethoxyflavones (PMFs) from Citrus genus because of their wide range of biological properties has been reported in various studies. Hydroxylated PMFs are unique flavones and recognized as the methoxy group of PMFs that is substituted for hydroxyl one. Hydroxylated PMFs are naturally existed in citrus peel and other plants as well as occurred as metabolites of their PMFs counterparts. Several in vitro and in vivo studies have documented the chemopreventive effects of hydroxylated PMFs including anti-cancer, anti-inflammation, anti-atherosclerosis, and neuroprotection. They function to regulate cell death, proliferation, differentiation, repair, and metabolism through acting on modulation of signaling cascade, gene transcription, and protein function and enzyme activity. The mechanisms of action of hydroxylated PMFs in disease chemoprevention depend on their structure, the number, and position of hydroxyl group. Although the efficacy of hydroxylated PMFs in chemoprevention and the oral bioavailability requires further investigation, they still provide great promise for improving human health. This review highlights the recent published data of hydroxylated PMFs with chemopreventive potential and the underlying mechanism involved. (c) 2015 BioFactors, 41(5):301-313, 2015.